Lead Definition
The LDC is active in the field of small molecule drug discovery striving to discover novel “leads”.
A lead is a well-characterized representative of a defined chemical compound class in the early phase of drug discovery with the potential to develop a drug from it.
Predominantly, a lead is derived from a primary “hit” – a compound active in a primary biological assay with a certain biological effect but yet without detailed characterization. A lead has already undergone the initial steps of optimization in medicinal chemistry. To qualify for nomination as a lead, an optimized compound series must meet certain specifications – the so-called lead criteria.
Currently, there is no generic definition for the term “lead” in the pharmaceutical industry, and different criteria are applied. Together with leading representatives of the industry, the LDC has established the following, commonly accepted lead criteria which characterize the product of a typical LDC project. LDC products have to fulfill strict requirements and thereby provide the basis for a swift optimization and smooth transition into clinical development.
LDC Lead Criteria
- Proof of concept in a relevant therapeutic or mechanistic animal model.
- Clear Mode of Action, as well as sufficient potency and selectivity.
- Clear Structure-Activity Relationship (SAR) and potential for further optimization.
- Appropriate physicochemical, biopharmaceutical and pharmacokinetic properties (SPR)
- Clear strategy for further optimization of the compound properties in the lead optimization phase.
- Intellectual property secured through initial patent applications or clear strategy to achieve Freedom to Operate.
